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Design and Synthesis of Novel N ‐(2‐aminophenyl)benzamide Derivatives as Histone Deacetylase Inhibitors and Their Antitumor Activity Study
Author(s) -
La Minh Thanh,
Jeong ByungHoon,
Kim HeeKwon
Publication year - 2021
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.12254
Subject(s) - benzamide , chemistry , histone deacetylase , apoptosis , in vivo , cancer research , pharmacology , cancer cell , cancer , histone , stereochemistry , biochemistry , biology , medicine , microbiology and biotechnology , gene
Histone deacetylases (HDACs) are promising therapeutic targets for cancer therapy because inhibition of HDACs triggers growth arrest or apoptosis of tumor cells. In the present study, a new series of fluorinated N ‐(2‐aminophenyl)benzamide derivatives were synthesized to investigate potential inhibition of HDACs and associated anticancer activity. Among the synthesized derivatives, compound 24a showed potent inhibitory activity of HDACs and higher antitumor efficacy in human cancer cell lines (HCT‐116, MCF‐7, and A549) compared with SAHA. Moreover, animal studies demonstrated that compound 24a showed potent in vivo antitumor efficacy in an HCT‐116 colon cancer xenograft mouse model.